Share this post on:

product name PAC-1


Description: First procaspase-activating compound (PAC-1) is a small-molecule activator of procaspase-3 that directly catalyzes the maturation of procaspase-3 to the active caspase-3 by inducing the cleavage of procaspase-3 in a time-dependent manner. Study results have demonstrated that PAC-1 is able to induce cell death in both primary cancerous cells and adjacent normal tissues with 50% inhibition concentration IC50 values ranging from 0.003 to 1.41 μM and 5.02 to 9.98 μM respectively.

Reference: Nat Chem Biol. 2006 Oct;2(10):543-50.



Molecular Weight (MW)

392.49
Formula

C23H28N4O2
CAS No.

315183-21-2
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 78 mg/mL (198.73 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: 16 mg/mL (40.76 mM)
Solubility (In vivo)

 30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL

other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19404850

General Administration of PAC-1 at 5 mg with low and steady releasing significantly inhibits the growth of ACHN renal cancer xenograft in mice. Oral administration of PAC-1 (50 or 100 mg/kg) significantly retards tumor growth of NCI-H226 lung cancer xenograft in a dose-dependent manner, and markedly prevents the cancer cells from infiltrating the lung tissue.
Animal model Mice s.c. injected with NCI-H226 (lung cancer) cells
Formulation Mixed with cholesterol and pelleted into a 3-mm-diameter 20-mg (total weight) pellet, or dissolved in a mixture of 24:1 vegetable oil/DMSO
Dosages 0, 50 or 100 mg/kg;
Administration p.o.; q.d., for 21 days
Reference [1] Putt KS, et al. Nat Chem Biol, 2006, 2(10), 543-550.

Gilteritinib